<p>Piceatannol (PCT), a fascinating compound found in plants, shows great potential in drug discovery. It proves to be a superior option, closely related to its well-known counterpart, resveratrol. Thus, updating all pharmaceutical aspects of this intriguing phytomolecule is essential. While resveratrol has stolen the limelight in scientific investigations, concerns have arisen regarding its practical application due to various limitations, such as poor bioavailability and unpredictable effects at different doses. Additionally, its interactions with other drugs, lack of standardization, and limited clinical evidence have cast doubts on its widespread use. PCT, the less investigated sibling, has been gaining momentum, boasting unique advantages over resveratrol and other stilbenoids. It showcases superior bioavailability and greater metabolic stability, suggesting that the body can more effectively utilize it. Moreover, its therapeutic profile holds great promise, surpassing that of resveratrol. This comprehensive review aims to provide updated information on all aspects of PCT, exploring its therapeutic potential, chemistry, biosynthesis, available formulation, pharmacokinetics parameters, and as well as its toxicity profile. It paves the way for a deeper understanding of this remarkable compound and opens doors to further scientific exploration.</p> Graphical abstract <p></p>